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Clinical data
Routes of
CAS Number
PubChem CID
ECHA InfoCard 100.233.599
Chemical and physical data
Formula C26H32N2O
Molar mass 388.25
3D model (JSmol)

Galeterone (developmental code names TOK-001, VN/124-1) is a novel steroid antiandrogen that was under development by Tokai Pharmaceuticals for the treatment of prostate cancer.[1] It possesses a unique dual mechanism of action, acting as both an androgen receptor antagonist and a CYP17A1 inhibitor, the latter of which prevents the biosynthesis of androgens.[2] As a CYP17A1 inhibitor, galeterone shows selectivity for 17,20-lyase over 17α-hydroxylase.[3]

Galeterone was being compared to enzalutamide in a phase III clinical trial (ARMOR3-SV) for AR-V7-expressing metastatic castration-resistant prostate cancer.[4][5] Tokai announced the discontinuation of ARMOR3-SV on July 26, 2016, after a data monitoring committee determined that the trial was unlikely to meet its endpoint.[6] On August 22, 2016, the company announced the discontinuation of their phase II expansion (ARMOR2) as well.[7]

In the week following cancellation of the ARMOR3-SV clinical trial, Tokai announced a reduction of its workforce by around 60% to a total of 10 "full-time equivalent employees."[8] On December 22, 2016, a definitive share purchase agreement was announced, under which shareholders of Otic Pharma Ltd. would become the majority owners of Tokai Pharmaceuticals Inc., resulting in a NASDAQ-listed company (OticPharma, Inc.) focused on the development and commercialization of products for ear, nose, and throat disorders.[9]

In August 2017, the development of galeterone was discontinued.[1]


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  2. ^ Brawer MK (2008). "New treatments for castration-resistant prostate cancer: highlights from the 44th annual meeting of the American Society of Clinical Oncology, May 30–June 3, 2008, Chicago, IL". Rev Urol. 10 (4): 294–6. PMC 2615106Freely accessible. PMID 19145273. 
  3. ^ Yin L, Hu Q (2014). "CYP17 inhibitors--abiraterone, C17,20-lyase inhibitors and multi-targeting agents". Nat Rev Urol. 11 (1): 32–42. doi:10.1038/nrurol.2013.274. PMID 24276076. 
  4. ^ "A Study of Galeterone Compared to Enzalutamide In Men Expressing Androgen Receptor Splice Variant-7 mRNA (AR-V7) Metastatic CRPC - Full Text View -". Retrieved 2016-02-27. 
  5. ^ Silberstein, John L.; Taylor, Maritza N.; Antonarakis, Emmanuel S. (2016-04-01). "Novel Insights into Molecular Indicators of Response and Resistance to Modern Androgen-Axis Therapies in Prostate Cancer". Current Urology Reports. 17 (4): 29. doi:10.1007/s11934-016-0584-4. ISSN 1534-6285. PMC 4888068Freely accessible. PMID 26902623. 
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